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Protein kinases as drug targets in cancer

Arslan, Mehmet Alper and Kütük, Özgür and Başağa, Hüveyda (2006) Protein kinases as drug targets in cancer. Current Cancer Drug Targets, 6 (7). pp. 623-634. ISSN 1568-0096

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Official URL: http://dx.doi.org/10.2174/156800906778742479

Abstract

Identification of the key roles of protein kinases in signaling pathways leading to development of cancer has caused pharmacological interest to concentrate extensively on targeted therapies as a more specific and effective way for blockade of cancer progression. This review will mainly focus on inhibitors targeting these key components of cellular signaling by employing a technology-based point of view with respect to ATP- and non-ATP-competitive small molecule inhibitors and monoclonal antibodies of selected protein kinases, particularly, mammalian target of rapamycin (mTOR), BCR-ABL, MEK, p38 MAPK, EGFR PDGFR, VEGFR, HER2 and Raf. Inhibitors of the heat shock protein Hsp90 are also included in a separate section, as this protein plays an essential role for the maturation/proper activation of cancer-related protein kinases. In the following review, the molecular details of the mode of action of these inhibitors as well as the emergence of drug resistance encountered in several cases are discussed in light of the structural, molecular and clinical studies conducted so far.

Item Type:Article
Uncontrolled Keywords:Rapamycin; ATP-Competitive inhibitors; BCR-ABL variants; Imatinib; Gastrointestinal stromal tumors (GIST); Monoclonal antibodies
Subjects:R Medicine > RC Internal medicine
ID Code:68
Deposited By:Alper Mehmet Arslan
Deposited On:04 Dec 2006 02:00
Last Modified:25 May 2011 14:02

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